6328-94-5Relevant academic research and scientific papers
Silver-Mediated Synthesis of 4H-Benzoxazin-4-ones by Intramolecular Decarboxylative O-Acylation Reactions with α-Oxocarboxylic Acid
Bharathimohan, Kuppusamy,Ponpandian, Thanasekaran,Jafar, Ahamed A.
, p. 2806 - 2813 (2017/05/29)
The first example of an intramolecular decarboxylative acylation reaction for the synthesis of 4H-benzoxazin-4-one derivatives has been described. The silver-mediated reaction has a broad substrate scope and provides a mild and rapid approach to the corre
Synthesis of a novel series of 2,3-disubstituted quinazolin-4(3H)-ones as a product of a nucleophilic attack at C(2) of the corresponding 4H-3,1-benzoxazin-4-one
El-Hashash, Mahr A.,El-Badry, Yaser A.
scheme or table, p. 389 - 396 (2011/04/25)
A new series of 2,3-disubstituted quinazolin-4(3H)-one derivatives was synthesized by nucleophilic attack at C(2) of the corresponding key starting material 2-propyl-4H-3,1-benzoxazin-4-one (Scheme 2). The reaction proceeded via amidinium salt formation (Scheme 3) rather than via an N-acylanthranilimide. The structure of the prepared compounds were elucidated by physical and spectral data like FTIR, 1H-NMR, and mass spectroscopy.
Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one
Kumar, Praveen,Shrivastava, Birendra,Pandeya, Surendra N.,Stables, James P.
experimental part, p. 1006 - 1018 (2011/04/24)
Thirty new 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one were designed and synthesized keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity of the titled compounds was assessed using the 6 Hz psychomotor seizure test. The most active compound of the series was 3-({(E)-[3-(4-chloro-3-methylphenoxy)phenyl]methylidene}amino) -2-phenylquinazolin-4(3H)-one PhQZ 7, which showed 100% protection (4/4, 0.5 h) and 75% protection (3/4, 0.25 h) at a dose of 100 mg/kg in mice. A computational study was carried out for calculation of pharmacophore pattern and prediction of pharmacokinetic properties. Titled compounds have also exhibited good binding properties with epilepsy molecular targets such as glutamate, GABA (A) delta and GABA (A) alpha-1 receptors, in Lamarckian genetic algorithm based flexible docking studies.
Synthesis and biological evaluation of some new 4(3H)-quinazolinone derivatives as non-classical antifolate
El-Hashash,El-Metwally,Eissa,El-Gohary
, p. 777 - 790 (2013/05/21)
LL living cell need tetrahydrofolate cofactor for the synthesis of purines, some amino acid and thymidine. Most bacteria and plant produce this folate cofactor by de novo biosynthesis. Compounds that interfere with this pathway, antifolate agents have found use as anticancer. Thus, the 2-propyl-4H-3,1- benzoxazin-4-one (2) was synthesized and allowed to interaction with Ammonium acetate or formamide afforded-2-propylquinazolin-4(3H)-one (3). Behaviour of quinazolinone towards carbon electrophiles namely, aromatic aldehyde, chloroacetylchloride, and ethylchloroacetate has been investigated and all the synthesized compounds were tested as anti-cancer in National Cancer Institute (NCI) in USA.
Methods and compositions utilizing quinazolinones
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, (2008/06/13)
Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
Process for the racemization of chiral quinazolinones
-
, (2008/06/13)
Racemates are obtained from one of the enantiomers, or an enantiomerically enriched mixture, of an optically active quinazolinone derivative by reaction of the compound with an alkali alkoxide of a primary alcohol and isolation of the racemate.
Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds
Segarra, Victor,Crespo, M. Isabel,Pujol, Ferran,Beleta, Jorge,Domenech, Teresa,Miralpeix, Montserrat,Palacios, Jose M.,Castro, Ana,Martinez, Ana
, p. 505 - 510 (2007/10/03)
A 4-centre PDE 4 pharmacophore search has been carried out in several 3D-databases containing compounds belonging to different therapeutic areas. Losartan, an angiotensin-II antagonist, has been identified as a new lead compound for developing PDE 4 inhibitors. New families of compounds derived from losartan has been synthesized and their PDE inhibition has been measured.
